反应 #872

ord-29bd294101a04d54b49813c6be393808

反应方程式

CCOC[C@H](NC(=O)[C@H](NC(=O)[C@@H](NC(=O)OCc1ccccc1)C(Cc1ccccc1)C(=O)O)C(C)C)c1ccccc1
N-benzyloxycarbonyl-β-benzyl-L-aspartyl-D-valine (R)-α-ethoxymethylbenzylamide
CCOC[C@H](NC(=O)[C@H](NC(=O)[C@@H](N)CC(=O)O)C(C)C)c1ccccc1
α-L-aspartyl-D-valine (R)-α-ethoxymethylbenzylamide
收率 50.3%

反应条件

温度
40°CELSIUS
详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    其他the catalyst was removed by filtration
  2. 2
    浓缩the resulting filtrate was concentrated under reduced pressure to 5 ml
  3. 3
    其他The crystal thus precipitated
  4. 4
    其他was removed by filtration
  5. 5
    其他dried

实验过程

To a suspension of 1.20 g (1.99 mmols) of N-benzyloxycarbonyl-β-benzyl-L-aspartyl-D-valine (R)-α-ethoxymethylbenzylamide in 50 ml of methanol and 10 ml of water was added 0.30 g of 10% Pd-carbon (water content 50%). The mixture was reduced under hydrogen under heat at 40°C., 40 ml of water was added thereto, the catalyst was removed by filtration, and the resulting filtrate was concentrated under reduced pressure to 5 ml. The crystal thus precipitated was removed by filtration and dried to obtain 0.38 g (1.00 mmol, 50.3%) of α-L-aspartyl-D-valine (R)-α-ethoxymethylbenzylamide.

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US05723165uspto-grants-1998_03